pethidine hydrochloride

CLINICAL USE

Opiate analgesia

DOSE IN NORMAL RENAL FUNCTION

IV: 25–50 mg every 4 hoursOral: 50–150 mg every 4 hoursS/C, IM: 25–100 mg every 4 hours

PHARMACOKINETICS

Molecular weight :283.8

%Protein binding :60–80

%Excreted unchanged in urine : 5

Volume of distribution (L/kg) :4.17

half-life – normal/ESRD (hrs) :3–6/7–32

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Use small doses – increase dosing interval to 6 hours and decrease dose by 25%

<10 : Avoid if possible. If not, use small doses: increase dosing interval to 8 hours and decrease dose by 50%

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in GFR <10 mL/min

HD :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux :Unknown dialysability. Dose as in GFR <10 mL/min

CAV/VVHD :Unlikely dialysability. Dose as in GFR 10 to 20 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anti-arrhythmics: delayed absorption of mexiletine

Antidepressants: possible CNS excitation or depression with MAOIs and moclobemide – avoid concomitant use; possibly increased serotonergic effects with duloxetine; increased sedative effects with tricyclics

Antipsychotics: enhanced sedative and hypotensive effect

Antivirals: concentration reduced by ritonavir but concentration of toxic pethidine metabolite increased – avoid concomitant use

Dopaminergics: risk of CNS toxicity with rasagiline – avoid concomitant use; hyperpyrexia and CNS toxicity reported with selegiline – avoid concomitant useSodium oxybate: enhanced effect of sodium oxybate – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

IV, oral, SC, IM

Rate of Administration

IV: Bolus 3–4 minutes

Comments

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OTHER INFORMATION

Risk of CNS and respiratory depression or convulsions, particularly in ERF patients receiving regular doses, due to accumulation of active metabolite, norpethidine. Norpethidine levels can be measured

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